CDK4/6 Inhibitor Development
Aberrant activation of cell cycle protein-dependent kinase 4 and 6 (CDK4/6) pathways (independent of mitogen signaling) leads to uncontrolled proliferation of breast cancer cells. At Alfa Cytology, we are at the forefront of innovative cancer research, with a keen focus on developing cutting-edge CDK4/6 inhibitors for the breast cancer therapy.
Introduction to CDK4/6 Inhibitor for Breast Cancer
Breast cancer is a complex and heterogeneous disease, with various molecular subtypes that exhibit distinct biological characteristics. Among the key molecular drivers of breast cancer pathogenesis is the CDK4/6 signaling pathway. This vital regulatory pathway controls cell cycle progression, and its dysregulation is frequently observed in breast cancer, particularly in the luminal subtypes.
Fig. 1 Regulation of cell cycle in breast cancer in CDK4/6 inhibitors. (Wang, X., et al. 2024)
CDK4/6 Inhibitor Development for Breast Cancer
The recognition of the pivotal role of the CDK4/6 pathway in breast cancer pathogenesis has led to the development of a new class of targeted therapies known as CDK4/6 inhibitors. These small-molecule drugs are designed to selectively and potently inhibit the activity of CDK4 and CDK6, thereby disrupting the uncontrolled cell cycle progression that drives cancer cell proliferation. By targeting the CDK4/6 pathway, CDK4/6 inhibitors have demonstrated remarkable efficacy in the treatment of breast cancer.
| NCT | Therapeutics | Phase |
| NCT01740427 | PALOMA-2 | |
| NCT01958021 | MONALEESA-2 | |
| NCT02246621 | MONARCH-3 | |
| NCT02278120 | MONALEESA-7 | |
| NCT03966898 | DAWNA-2 | |
| NCT02422615 | MONALEESA-3 | |
| NCT02690480 | FLIPPER | |
| NCT03184090 | BioPER | |
| NCT03839823 | RIGHT |
Our Services
At Alfa Cytology, we have tried to identify different compounds with increased CDK4/6 selectivity, reduced adverse effects while maintaining or improving treatment efficacy for breast cancer. Our team has a deep understanding of the complex mechanisms underlying breast cancer, allowing us to develop innovative and targeted therapeutic strategies.
Select CDK4/6 Inhibitors Development
- Screening and identifying novel small molecule compounds that selectively inhibit CDK4 and CDK6
- Improving potency, selectivity, metabolic stability, solubility, and other key parameters to develop drug-like CDK4/6 inhibitor candidates.
- Optimizing the pharmacokinetic, pharmacodynamic, and safety profiles of lead CDK4/6 inhibitor candidates
CDK4/6 Protein Degraders Development
- Designing bifunctional molecules that can simultaneously bind to CDK4/6 and recruit E3 ubiquitin ligases
- Leveraging targeted protein degradation to selectively eliminate CDK4/6 in cancer cells
- Developing optimized CDK4/6 protein degrader compounds with improved potency, selectivity, and drug-like properties
Our Advantages
- Have a large library of compounds
- Optimize and improve candidate CDK4/6 inhibitors
- Study of ligand-receptor interactions with accuracy and precision
- Rich breast cancer models
- Advanced high-throughput screening platform
- Provide full-stop service from drug discovery to preclinical service
Alfa Cytology provides development services for CDK4/6 inhibitors, covering drug design, screening, and efficacy research to find ideal drug candidates for you and accelerate preclinical research on your breast cancer therapeutics. These results can guide further drug optimization, reasonable dose selection, and preclinical drug safety evaluation. If you are interested in our service, please contact us.
Reference
- Wang, X., Zhao, S., and et al. Recent progress of CDK4/6 inhibitors' current practice in breast cancer. Cancer Gene Ther. 2024.